Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Research, Society and Development |
Texto Completo: | https://rsdjournal.org/index.php/rsd/article/view/8817 |
Resumo: | The objective of this work was to evaluate the antiplasmodial activity and toxicity of the extract and fractions obtained from the bark of Aspidosperma nitidum. The ethanol extract obtained from the powdered bark of plants was acid-base partitioned and phytochemically analyzed. The antiplasmodial activity, in vivo antimalarial activity and in vitro cytotoxicity were acessed. The selectivity index (SI) was calculated. The acute oral toxicity and pathological effects, of the ethanol extract was evaluated in mice. The major constituent of the ethanol extract was suggestive of a β-carboline chromophore. The alkaloid and neutral fractions contained compounds with an aspidospermine core as the major constituent. The ethanol extract (IC50 = 3.60 µg/mL), neutral fraction (IC50 = 3.34 µg/mL) and alkaloid fraction (IC50= 2.32 µg/mL) showed high activity against P. falciparum (W2 strain). The ethanol extract and the alkaloid fraction reduced 80% of the parasitemia of P. berghei (ANKA)-infected mice (dose of 500 mg/kg) in the 5th day, which was not sustainable at the 8th day. A similar result was obtained for chloroquine. The ethanol extract (CC50 = 410.65 µg/mL; SI = 114.07), neutral fraction (CC50 = 452.53 µg/mL; SI = 135.49), and alkaloid fraction (CC50 =346.73 µg/mL; SI 149.45) demonstrated low cytotoxicity and high SI. The ethanol extract (5000 mg/kg; gavage) presented low acute oral toxicity, with no clinical or anatomopathological modifications being observed (in comparison to the control group). In vitro studies with a chloroquine-resistant clone of P. falciparum confirmed the antiplasmodial activity of the A. nitidum ethanol extract, and its fractions had low cytotoxicity for HepG2 cells. In vivo studies with P. berghei–infected mice and acute toxicity studies corroborated these results. |
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Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon Actividad antipalúdica y toxicidad de Aspidosperma nitidum Benth: una planta utilizada en la medicina tradicional en la Amazonía brasileña Atividade antimalárica e toxicidade de Aspidosperma nitidum Benth: uma planta usada na medicina tradicional na Amazônia brasileiraApocynaceaeAspidosperma nitidumMalariaToxicity.ApocynaceaeAspidosperma nitidumMalariaToxicidad.ApocynaceaeAspidosperma nitidumMalariaToxicidade.The objective of this work was to evaluate the antiplasmodial activity and toxicity of the extract and fractions obtained from the bark of Aspidosperma nitidum. The ethanol extract obtained from the powdered bark of plants was acid-base partitioned and phytochemically analyzed. The antiplasmodial activity, in vivo antimalarial activity and in vitro cytotoxicity were acessed. The selectivity index (SI) was calculated. The acute oral toxicity and pathological effects, of the ethanol extract was evaluated in mice. The major constituent of the ethanol extract was suggestive of a β-carboline chromophore. The alkaloid and neutral fractions contained compounds with an aspidospermine core as the major constituent. The ethanol extract (IC50 = 3.60 µg/mL), neutral fraction (IC50 = 3.34 µg/mL) and alkaloid fraction (IC50= 2.32 µg/mL) showed high activity against P. falciparum (W2 strain). The ethanol extract and the alkaloid fraction reduced 80% of the parasitemia of P. berghei (ANKA)-infected mice (dose of 500 mg/kg) in the 5th day, which was not sustainable at the 8th day. A similar result was obtained for chloroquine. The ethanol extract (CC50 = 410.65 µg/mL; SI = 114.07), neutral fraction (CC50 = 452.53 µg/mL; SI = 135.49), and alkaloid fraction (CC50 =346.73 µg/mL; SI 149.45) demonstrated low cytotoxicity and high SI. The ethanol extract (5000 mg/kg; gavage) presented low acute oral toxicity, with no clinical or anatomopathological modifications being observed (in comparison to the control group). In vitro studies with a chloroquine-resistant clone of P. falciparum confirmed the antiplasmodial activity of the A. nitidum ethanol extract, and its fractions had low cytotoxicity for HepG2 cells. In vivo studies with P. berghei–infected mice and acute toxicity studies corroborated these results.El objetivo de este trabajo fue evaluar la actividad antiplasmodial y la toxicidad del extracto y fracciones obtenidas de la corteza de Aspidosperma nitidum. El extracto de etanol obtenido de la corteza en polvo de plantas se repartió ácido-base y se analizó fitoquímicamente. Se redujeron la actividad antiplasmodial, la actividad antipalúdica in vivo y la citotoxicidad in vitro. Se calculó el índice de selectividad (SI). Se evaluó la toxicidad oral aguda y los efectos patológicos del extracto de etanol en ratones. El componente principal del extracto de etanol sugirió un cromóforo de β-carbolina. Las fracciones alcaloide y neutra contenían compuestos con un núcleo de aspidospermina como constituyente principal. El extracto de etanol (CI50 = 3.60 µg / mL), la fracción neutra (CI50 = 3.34 µg / mL) y la fracción alcaloide (CI50 = 2.32 µg / mL) mostraron alta actividad contra P. falciparum (cepa W2). El extracto de etanol y la fracción alcaloide redujeron el 80% de la parasitemia de ratones infectados con P. berghei (ANKA) (dosis de 500 mg / kg) en el quinto día, lo que no fue sostenible en el octavo día. Se obtuvo un resultado similar para la cloroquina. El extracto de etanol (CC50 = 410.65 µg / mL; SI = 114.07), fracción neutra (CC50 = 452.53 µg / mL; SI = 135.49) y fracción alcaloide (CC50 = 346.73 µg / mL; SI 149.45) demostraron citotoxicidad baja y alta SI. El extracto de etanol (5000 mg / kg; sonda) presentó baja toxicidad oral aguda, sin observarse modificaciones clínicas ni anatomopatológicas (en comparación con el grupo control). Los estudios in vitro con un clon de P. falciparum resistente a la cloroquina confirmaron la actividad antiplasmodial del extracto etanólico de A. nitidum, y sus fracciones tenían baja citotoxicidad para las células HepG2. Los estudios in vivo con ratones infectados por P. berghei y los estudios de toxicidad aguda corroboraron estos resultados.O objetivo deste trabalho foi avaliar a atividade antiplasmódica e a toxicidade do extrato e frações obtidas da casca de Aspidosperma nitidum. O extrato etanólico obtido dos pós da casca da planta e foi particionado ácido-base e analisado fitoquimicamente. Foram avaliadas a atividade antiplasmódica, atividade antimalárica in vivo e citotoxicidade in vitro. O índice de seletividade (SI) foi calculado. A toxicidade oral aguda e os efeitos patológicos do extrato etanólico foram avaliados em camundongos. O principal constituinte do extrato etanólico foi sugestivo de um cromóforo β-carbolina. As frações alcalóide e neutra continham compostos com um núcleo de aspidospermina como principal constituinte. O extrato etanólico (IC50 = 3,60 µg / mL), fração neutra (IC50 = 3,34 µg / mL) e a fração alcalóide (IC50 = 2,32 µg / mL) apresentaram alta atividade contra P. falciparum (cepa W2). O extrato etanólico e a fração alcalóide reduziram em 80% a parasitemia de camundongos infectados com P. berghei (ANKA) (dose de 500 mg / kg) no 5º dia, o que não foi sustentável no 8º dia. Um resultado semelhante foi obtido para a cloroquina. O extrato de etanol (CC50 = 410,65 µg / mL; SI = 114,07), fração neutra (CC50 = 452,53 µg / mL; SI = 135,49) e fração alcalóide (CC50 = 346,73 µg / mL; SI 149,45) demonstrou baixa citotoxicidade e alta SI. O extrato etanólico (5000 mg / kg; gavagem) apresentou baixa toxicidade oral aguda, não sendo observadas modificações clínicas ou anatomopatológicas (em comparação ao grupo controle). Estudos in vitro com um clone de P. falciparum resistente à cloroquina confirmaram a atividade antiplasmódica do extrato etanólico de A. nitidum, e suas frações apresentaram baixa citotoxicidade para células HepG2. Estudos in vivo com camundongos infectados por P. berghei e estudos de toxicidade aguda corroboraram esses resultados.Research, Society and Development2020-10-05info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://rsdjournal.org/index.php/rsd/article/view/881710.33448/rsd-v9i10.8817Research, Society and Development; Vol. 9 No. 10; e5059108817Research, Society and Development; Vol. 9 Núm. 10; e5059108817Research, Society and Development; v. 9 n. 10; e50591088172525-3409reponame:Research, Society and Developmentinstname:Universidade Federal de Itajubá (UNIFEI)instacron:UNIFEIenghttps://rsdjournal.org/index.php/rsd/article/view/8817/7860Copyright (c) 2020 Dayse Lucia do Nascimento Brandão; Michel Tavares Martins; Adreanne Oliveira Silva; Amanda Dias Almeida; Renata Cristina de Paula; Alaíde Braga de Oliveira; Marlia Regina Coelho-Ferreira; Antonio Taylon Aguiar Gomes; Flavio de Vasconcelos; Washington Luiz Assunção Pereira; Valdicley Vieira Vale; Sandro Percário; Maria Fâni Dolabelahttps://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessBrandão, Dayse Lucia do Nascimento Martins, Michel TavaresSilva, Adreanne Oliveira Almeida, Amanda Dias Paula, Renata Cristina de Oliveira, Alaíde Braga de Coelho-Ferreira, Marlia ReginaGomes, Antonio Taylon Aguiar Vasconcelos, Flavio dePereira, Washington Luiz Assunção Vale, Valdicley Vieira Percário, SandroDolabela, Maria Fâni 2020-10-31T12:03:23Zoai:ojs.pkp.sfu.ca:article/8817Revistahttps://rsdjournal.org/index.php/rsd/indexPUBhttps://rsdjournal.org/index.php/rsd/oairsd.articles@gmail.com2525-34092525-3409opendoar:2024-01-17T09:31:12.408882Research, Society and Development - Universidade Federal de Itajubá (UNIFEI)false |
dc.title.none.fl_str_mv |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon Actividad antipalúdica y toxicidad de Aspidosperma nitidum Benth: una planta utilizada en la medicina tradicional en la Amazonía brasileña Atividade antimalárica e toxicidade de Aspidosperma nitidum Benth: uma planta usada na medicina tradicional na Amazônia brasileira |
title |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon |
spellingShingle |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon Brandão, Dayse Lucia do Nascimento Apocynaceae Aspidosperma nitidum Malaria Toxicity. Apocynaceae Aspidosperma nitidum Malaria Toxicidad. Apocynaceae Aspidosperma nitidum Malaria Toxicidade. |
title_short |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon |
title_full |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon |
title_fullStr |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon |
title_full_unstemmed |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon |
title_sort |
Anti-malarial activity and toxicity of Aspidosperma nitidum Benth: a plant used in traditional medicine in the Brazilian Amazon |
author |
Brandão, Dayse Lucia do Nascimento |
author_facet |
Brandão, Dayse Lucia do Nascimento Martins, Michel Tavares Silva, Adreanne Oliveira Almeida, Amanda Dias Paula, Renata Cristina de Oliveira, Alaíde Braga de Coelho-Ferreira, Marlia Regina Gomes, Antonio Taylon Aguiar Vasconcelos, Flavio de Pereira, Washington Luiz Assunção Vale, Valdicley Vieira Percário, Sandro Dolabela, Maria Fâni |
author_role |
author |
author2 |
Martins, Michel Tavares Silva, Adreanne Oliveira Almeida, Amanda Dias Paula, Renata Cristina de Oliveira, Alaíde Braga de Coelho-Ferreira, Marlia Regina Gomes, Antonio Taylon Aguiar Vasconcelos, Flavio de Pereira, Washington Luiz Assunção Vale, Valdicley Vieira Percário, Sandro Dolabela, Maria Fâni |
author2_role |
author author author author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Brandão, Dayse Lucia do Nascimento Martins, Michel Tavares Silva, Adreanne Oliveira Almeida, Amanda Dias Paula, Renata Cristina de Oliveira, Alaíde Braga de Coelho-Ferreira, Marlia Regina Gomes, Antonio Taylon Aguiar Vasconcelos, Flavio de Pereira, Washington Luiz Assunção Vale, Valdicley Vieira Percário, Sandro Dolabela, Maria Fâni |
dc.subject.por.fl_str_mv |
Apocynaceae Aspidosperma nitidum Malaria Toxicity. Apocynaceae Aspidosperma nitidum Malaria Toxicidad. Apocynaceae Aspidosperma nitidum Malaria Toxicidade. |
topic |
Apocynaceae Aspidosperma nitidum Malaria Toxicity. Apocynaceae Aspidosperma nitidum Malaria Toxicidad. Apocynaceae Aspidosperma nitidum Malaria Toxicidade. |
description |
The objective of this work was to evaluate the antiplasmodial activity and toxicity of the extract and fractions obtained from the bark of Aspidosperma nitidum. The ethanol extract obtained from the powdered bark of plants was acid-base partitioned and phytochemically analyzed. The antiplasmodial activity, in vivo antimalarial activity and in vitro cytotoxicity were acessed. The selectivity index (SI) was calculated. The acute oral toxicity and pathological effects, of the ethanol extract was evaluated in mice. The major constituent of the ethanol extract was suggestive of a β-carboline chromophore. The alkaloid and neutral fractions contained compounds with an aspidospermine core as the major constituent. The ethanol extract (IC50 = 3.60 µg/mL), neutral fraction (IC50 = 3.34 µg/mL) and alkaloid fraction (IC50= 2.32 µg/mL) showed high activity against P. falciparum (W2 strain). The ethanol extract and the alkaloid fraction reduced 80% of the parasitemia of P. berghei (ANKA)-infected mice (dose of 500 mg/kg) in the 5th day, which was not sustainable at the 8th day. A similar result was obtained for chloroquine. The ethanol extract (CC50 = 410.65 µg/mL; SI = 114.07), neutral fraction (CC50 = 452.53 µg/mL; SI = 135.49), and alkaloid fraction (CC50 =346.73 µg/mL; SI 149.45) demonstrated low cytotoxicity and high SI. The ethanol extract (5000 mg/kg; gavage) presented low acute oral toxicity, with no clinical or anatomopathological modifications being observed (in comparison to the control group). In vitro studies with a chloroquine-resistant clone of P. falciparum confirmed the antiplasmodial activity of the A. nitidum ethanol extract, and its fractions had low cytotoxicity for HepG2 cells. In vivo studies with P. berghei–infected mice and acute toxicity studies corroborated these results. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-10-05 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://rsdjournal.org/index.php/rsd/article/view/8817 10.33448/rsd-v9i10.8817 |
url |
https://rsdjournal.org/index.php/rsd/article/view/8817 |
identifier_str_mv |
10.33448/rsd-v9i10.8817 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://rsdjournal.org/index.php/rsd/article/view/8817/7860 |
dc.rights.driver.fl_str_mv |
https://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
https://creativecommons.org/licenses/by/4.0 |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Research, Society and Development |
publisher.none.fl_str_mv |
Research, Society and Development |
dc.source.none.fl_str_mv |
Research, Society and Development; Vol. 9 No. 10; e5059108817 Research, Society and Development; Vol. 9 Núm. 10; e5059108817 Research, Society and Development; v. 9 n. 10; e5059108817 2525-3409 reponame:Research, Society and Development instname:Universidade Federal de Itajubá (UNIFEI) instacron:UNIFEI |
instname_str |
Universidade Federal de Itajubá (UNIFEI) |
instacron_str |
UNIFEI |
institution |
UNIFEI |
reponame_str |
Research, Society and Development |
collection |
Research, Society and Development |
repository.name.fl_str_mv |
Research, Society and Development - Universidade Federal de Itajubá (UNIFEI) |
repository.mail.fl_str_mv |
rsd.articles@gmail.com |
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1797052741245206528 |